(Z)-N'-(2-hydroxy-3-(piperidin-1-yl)propoxy)nicotiniMidaMide

BGP-15 (66611-37-8) is a cellular protectant operating by several mechanisms. It is an insulin sensitizer1, HSP72 activator2, PARP inhibitor and ROS and lipid peroxidation reducer3. It protects mitochondria in acetaminophen-induced liver injury4 as well as LPS-induced destabilization5 and activates mitochondrial fusion6. Displays protective effects in heart failure7 and traumatic brain injury8 in animal models.

BGP 15 is a calcipotriene-based vitamin D3 analog that inhibits poly(ADP-ribose) polymerasesis (PARP), a class of enzymes that regulate DNA repair and apoptosis (1). BGP 15 is also a cardioprotective agent (2). Also, BPG 15 improves mitochondrial function, protects neurons from dying in vitro and in vivo, and promotes cardiac innervation in vivo.

previous study showed that bgp-15 at 200 μm could prevent the imatinib-induced oxidative damages, attenuate the depletion of high-energy phosphates, alter the signaling effect of imatinib by preventing p38 map kinase and jnk activation, and also induce the akt and gsk-3β phosphorylation [1].

in-vivo study indicated that bgp-15 improved cardiac function and reduced arrhythmic episodes in two hf and af mouse models. in these models, bgp-15 was associated with increased phosphorylation of igf1r. moreover, cardiac-specific igf1r transgenic overexpression in mice recapitulated the protection caused by bgp-15. the authors further demonstrated that bgp-15 with igf1r could provide protection independent of phosphoinositide 3-kinase-akt and heat-shock protein 70 [2].

PARP: 120 μM (IC₅₀)

Store at -20°C

[1] ÁGOTA PETŐ. Pharmacological Overview of the BGP-15 Chemical Agent as a New Drug Candidate for the Treatment of Symptoms of Metabolic Syndrome.[J]. Molecules, 2020, 25 2. DOI:10.3390/molecules25020429
[2] DARREN C HENSTRIDGE. Activating HSP72 in rodent skeletal muscle increases mitochondrial number and oxidative capacity and decreases insulin resistance.[J]. ACS Applied Nano Materials, 2014: 1881-1894. DOI:10.2337/db13-0967
[3] ESZTER SZABADOS . BGP-15, a nicotinic amidoxime derivate protecting heart from ischemia reperfusion injury through modulation of poly(ADP-ribose) polymerase[J]. Biochemical pharmacology, 2000, 59 8: Pages 937-945. DOI:10.1016/s0006-2952(99)00418-9
[4] FARKAS SARNYAI. BGP-15 Protects Mitochondria in Acute, Acetaminophen Overdose Induced Liver Injury[J]. Pathology & Oncology Research, 2019, 24 1: 1797-1803. DOI:10.1007/s12253-019-00721-1
[5] KATALIN SUMEGI. BGP-15 Protects against Oxidative Stress- or Lipopolysaccharide-Induced Mitochondrial Destabilization and Reduces Mitochondrial Production of Reactive Oxygen Species[J]. PLoS ONE, 2017. DOI:10.1371/journal.pone.0169372
[6] ALIZ SZABO . Activation of mitochondrial fusion provides a new treatment for mitochondria-related diseases[J]. Biochemical pharmacology, 2018, 150: Pages 86-96. DOI:10.1016/j.bcp.2018.01.038
[7] GEETA SAPRA. The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice.[J]. Nature Communications, 2014: 5705. DOI:10.1038/ncomms6705
[8] BINNUR EROGLU. Therapeutic inducers of the HSP70/HSP110 protect mice against traumatic brain injury[J]. Journal of Neurochemistry, 2014, 130 5: 626-641. DOI:10.1111/jnc.12781